AR050932A1 - BICYCLE AMIDAS AS CINASE INHIBITORS - Google Patents

BICYCLE AMIDAS AS CINASE INHIBITORS

Info

Publication number
AR050932A1
AR050932A1 ARP050103817A ARP050103817A AR050932A1 AR 050932 A1 AR050932 A1 AR 050932A1 AR P050103817 A ARP050103817 A AR P050103817A AR P050103817 A ARP050103817 A AR P050103817A AR 050932 A1 AR050932 A1 AR 050932A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
lower alkyl
alkylene
independently selected
Prior art date
Application number
ARP050103817A
Other languages
Spanish (es)
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0420520A external-priority patent/GB0420520D0/en
Priority claimed from GB0511687A external-priority patent/GB0511687D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR050932A1 publication Critical patent/AR050932A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

La presente se refiere a compuestos de formula (1), a composiciones farmacéuticas que los comprenden y a su uso en el tratamiento de enfermedades dependientes de cinasa de proteína, especialmente enfermedades proliferativas, en particular enfermedades tumorales. Reivindicacion 1: Un compuesto de la formula (1) en donde R1 es H, halogeno, ciano, -C0-C7-O-R3; -C0-C7-NR4R5, o -C(=O)-R6; R2 es cicloalquilo C3-8 substituido; arilo substituido; o heterociclilo substituido; R3 es H o alquilo inferior no substituido o substituido; R4 y R5 se seleccionan independientemente del grupo que consiste de H, alquilo inferior no substituido o substituido, alquilcarbonilo inferior, en donde la porcion de alquilo inferior está opcionalmente substituida, y alcoxi-carbonilo inferior, en donde la porcion alquilo inferior está opcionalmente substituid; R6 es H, alquilo inferior no substituido o substituido, alcoxi inferior, en donde la porcion de alquilo inferior está opcionalmente substituida; amino no substituido, mono- o di-substituido; A, B, y X se seleccionan independientemente de =C(R7)- o N; E, G y T se seleccionan independientemente de =C(R9)- o N; R7 y R8 se seleccionan independientemente del grupo que consiste de H, halogeno y alquilo inferior no substituido o substituido; Y es -O-, -S-, -S(O)-, -S(O)2-, -CH2-, -CH2CH2-, -CH=CH- o -C:::C-; Z es CH o N y Q es alquileno C1-4 o alquenileno C2-4, en donde el alquileno C1-4 o el alquenileno C2-4 opcionalmente puede estar substituido y en donde uno o más de los átomos de C de dicha cadena de alquileno C1-4 o el alquenileno C2-4 opcionalmente puede ser reemplazado por un átomo heterogéneo independientemente seleccionado de H, O y S; y el enlace entre Q y Z caracterizado por una línea punteada es un enlace individual; siempre que si Z es N, Q no es un alquileno C2-4 no ramificado no substituido; o Z es C y Q como se definio anteriormente en donde el enlace entre Q y Z caracterizado por la línea punteada es un enlace doble; y W no está presente o es alquileno C1-3, o un tautomero del mismo, o una sal del mismo.This refers to compounds of formula (1), pharmaceutical compositions comprising them and their use in the treatment of protein kinase dependent diseases, especially proliferative diseases, in particular tumor diseases. Claim 1: A compound of the formula (1) wherein R1 is H, halogen, cyano, -C0-C7-O-R3; -C0-C7-NR4R5, or -C (= O) -R6; R2 is substituted C3-8 cycloalkyl; substituted aryl; or substituted heterocyclyl; R3 is H or unsubstituted or substituted lower alkyl; R4 and R5 are independently selected from the group consisting of H, unsubstituted or substituted lower alkyl, lower alkylcarbonyl, wherein the lower alkyl portion is optionally substituted, and lower alkoxycarbonyl, wherein the lower alkyl portion is optionally substituted; R6 is H, unsubstituted or substituted lower alkyl, lower alkoxy, wherein the lower alkyl portion is optionally substituted; unsubstituted, mono- or di-substituted amino; A, B, and X are independently selected from = C (R7) - or N; E, G and T are independently selected from = C (R9) - or N; R7 and R8 are independently selected from the group consisting of H, halogen and unsubstituted or substituted lower alkyl; Y is -O-, -S-, -S (O) -, -S (O) 2-, -CH2-, -CH2CH2-, -CH = CH- or -C ::: C-; Z is CH or N and Q is C1-4 alkylene or C2-4 alkenylene, wherein C1-4 alkylene or C2-4 alkenylene may optionally be substituted and where one or more of the C atoms of said chain of C1-4 alkylene or C2-4 alkenylene may optionally be replaced by a heterogeneous atom independently selected from H, O and S; and the link between Q and Z characterized by a dotted line is an individual link; provided that if Z is N, Q is not an unsubstituted unsubstituted C2-4 alkylene; or Z is C and Q as defined above where the link between Q and Z characterized by the dotted line is a double bond; and W is not present or is C1-3 alkylene, or a tautomer thereof, or a salt thereof.

ARP050103817A 2004-09-15 2005-09-13 BICYCLE AMIDAS AS CINASE INHIBITORS AR050932A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0420520A GB0420520D0 (en) 2004-09-15 2004-09-15 Organic compounds
GB0511687A GB0511687D0 (en) 2005-06-08 2005-06-08 Organic compounds

Publications (1)

Publication Number Publication Date
AR050932A1 true AR050932A1 (en) 2006-12-06

Family

ID=35705284

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050103817A AR050932A1 (en) 2004-09-15 2005-09-13 BICYCLE AMIDAS AS CINASE INHIBITORS

Country Status (23)

Country Link
US (2) US8026247B2 (en)
EP (1) EP1794149A2 (en)
JP (2) JP4950889B2 (en)
KR (3) KR20100111324A (en)
CN (1) CN101693709A (en)
AR (1) AR050932A1 (en)
AU (2) AU2005310968C1 (en)
BR (1) BRPI0515446A (en)
CA (2) CA2574829C (en)
EC (1) ECSP077324A (en)
GT (1) GT200500260A (en)
IL (1) IL181720A0 (en)
MA (1) MA28876B1 (en)
MX (1) MX2007003013A (en)
MY (2) MY147640A (en)
NO (1) NO20071875L (en)
NZ (3) NZ587806A (en)
PE (1) PE20060664A1 (en)
RU (3) RU2416611C2 (en)
SG (1) SG155921A1 (en)
TN (1) TNSN07093A1 (en)
TW (1) TW200626576A (en)
WO (1) WO2006059234A2 (en)

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